Muscarinic acetylcholine receptor

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Transcript of Muscarinic acetylcholine receptor

Complications faced when targeting the M1 receptorAmino acid sequences are highly conserved among the orthosteric binding sites in the five mAChRs (Eglen, Guatam, Wess)Non-selective targeting of the M1 receptor leads to several consequencesGI distressBradycardia (slow heart rate)Experimental Evidence of mAChR's ValueJ.J. Hagan, J.H. Jansen, C.L. Broekkamp (1987)Muscarinic Acetylcholine Receptors (mAChR)What is a mAChR? Research in Alzheimer's PatientsAbnormal Activity and Alzheimer's DiseaseIncreasing SelectivityAmino acid sequences are not conserved among the allosteric binding sites

Developed drugs that were allosteric agonists of the M1 receptorused M1 mAChR antagonist to block M1's function in rats rats showed impaired cognitive ability to memorize spatial map of maze-Xanomeline is an m1 and m4 agonist (similar to a ligand)